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A novel small-molecule inhibitor of IL-6 signalling |
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| Authors: | Zinzalla Giovanna Haque Mohammad R Basu B Piku Anderson John Kaye Samantha L Haider Shozeb Hasan Fyeza Antonow Dyeison Essex Samantha Rahman Khondaker M Palmer Jonathan Morgenstern Daniel Wilderspin Andrew F Neidle Stephen Thurston David E |
| Affiliation: | Cancer Research UK Protein, The School of Pharmacy, University of London, London, United Kingdom. |
| Abstract: | A small library of pyrrolidinesulphonylaryl molecules has been synthesized via an efficient 4-step route, and members evaluated for their ability to inhibit IL-6 signalling. One molecule (6a) was found to have promising activity against IL-6/STAT3 signalling at the low micromolar level, and to selectively inhibit phosphorylation of STAT3 (but not STAT1) in IL-6 stimulated MDA-MB-231 breast cancer and HeLa cell lines. It was also selectively cytostatic in MDA-MB-231 (STAT3-dependent) versus A4 (STAT3-null) cells suggesting STAT3-specific inhibitory properties. |
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